去甲基氟硝西泮
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| 法律規範狀態 | |
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| 法律規範 |
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| 识别信息 | |
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| CAS号 | 2558-30-7 |
| PubChem CID | |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.018.072 |
| 化学信息 | |
| 化学式 | C15H10FN3O3 |
| 摩尔质量 | 299.26 g·mol−1 |
| 3D模型（JSmol） | |
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去甲基氟硝西泮（英语：Desmethylflunitrazepam或Norflunitrazepam、开发代号：Ro05-4435），也叫Fonazepam，误译作去甲基氟西泮，是一种苯二氮䓬类药物，是氟硝西泮的代谢产物，[1][2][3]已作为设计师药物在网上销售。[4][5]它对GABAA受体的IC50值为1.499 nM。[6][7]
参见
参考资料
- ^ Busker RW, van Henegouwen GM, Kwee BM, Winkens JH. Photobinding of flunitrazepam and its major photo-decomposition product N-desmethylflunitrazepam. International Journal of Pharmaceutics. May 1987, 36 (2–3): 113–120. doi:10.1016/0378-5173(87)90145-1.
- ^ Coller JK, Somogyi AA, Bochner F. Quantification of flunitrazepam's oxidative metabolites, 3-hydroxyflunitrazepam and desmethylflunitrazepam, in hepatic microsomal incubations by high-performance liquid chromatography. Journal of Chromatography. B, Biomedical Sciences and Applications. November 1998, 719 (1–2): 87–92. PMID 9869368. doi:10.1016/S0378-4347(98)00383-1.
- ^ Kilicarslan T, Haining RL, Rettie AE, Busto U, Tyndale RF, Sellers EM. Flunitrazepam metabolism by cytochrome P450S 2C19 and 3A4. Drug Metabolism and Disposition. April 2001, 29 (4 Pt 1): 460–5. PMID 11259331.
- ^ Moosmann B, Bisel P, Franz F, Huppertz LM, Auwärter V. Characterization and in vitro phase I microsomal metabolism of designer benzodiazepines - an update comprising adinazolam, cloniprazepam, fonazepam, 3-hydroxyphenazepam, metizolam and nitrazolam. Journal of Mass Spectrometry. November 2016, 51 (11): 1080–1089. Bibcode:2016JMSp...51.1080M. PMID 27535017. doi:10.1002/jms.3840.
- ^ Katselou M, Papoutsis I, Nikolaou P, Spiliopoulou C, Athanaselis S. Metabolites replace the parent drug in the drug arena. The cases of fonazepam and nifoxipam. Forensic Toxicology. 2016, 35 (1): 1–10. PMC 5214877
. PMID 28127407. doi:10.1007/s11419-016-0338-5.
- ^ Maddalena DJ, Johnston GA. Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks. Journal of Medicinal Chemistry. February 1995, 38 (4): 715–24. PMID 7861419. doi:10.1021/jm00004a017.
- ^ So SS, Karplus M. Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors. Journal of Medicinal Chemistry. December 1996, 39 (26): 5246–56. PMID 8978853. doi:10.1021/jm960536o.
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